title: Exploring 8-benzyl pteridine-6,7-diones as inhibitors of glutamate racemase (MurI) in gram-positive bacteria.
abstract: A successful scaffold-hopping approach gave a novel series of inhibitors of bacterial glutamate racemase (MurI). Early SAR studies of the 8-benzyl pteridine-6,7-diones led to compounds with micromolar enzyme potency and antibacterial activity.
authors.affiliation: Infection Discovery, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA. gloria.breault@astrazeneca.com
authors.forename: Gloria A
authors.initials: GA
authors.lastname: Breault
authors.forename: Janelle
authors.initials: J
authors.lastname: Comita-Prevoir
authors.forename: Charles J
authors.initials: CJ
authors.lastname: Eyermann
authors.forename: Bolin
authors.initials: B
authors.lastname: Geng
authors.forename: Randy
authors.initials: R
authors.lastname: Petrichko
authors.forename: Peter
authors.initials: P
authors.lastname: Doig
authors.forename: Elise
authors.initials: E
authors.lastname: Gorseth
authors.forename: Brian
authors.initials: B
authors.lastname: Noonan
mesh_terms: D000591:Amino Acid Isomerases / Q000037:antagonists & inhibitors*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D006094:Gram-Positive Bacteria / Q000187:drug effects / Q000201:enzymology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011621:Pteridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: C534102:8-benzyl pteridine-6,7-dione; D000900:Anti-Bacterial Agents; D011621:Pteridines; D000591:Amino Acid Isomerases; C062292:glutamate racemase